POWDERED DOSAGE FORM

Powdererd dosage form can be classified into the followings

1. bulk powders for external use – termed dusting powders
2. bulk oral powders
3. individual unit dose powders
4. unit dose capsules.

Bulk powders for external use

These are dry, free-flowing preparations consisting of one or a mixture of finely
powdered substances and intended for external application.

The advantages of dusting powders as pharmaceutical products are as follows:

* They are easy to apply.
* They are pleasant to use.
* They absorb skin moisture, which leads to reduced friction between skin surfaces,
discourages bacterial growth and has a cooling effect.

The disadvantages of dusting powders as pharmaceutical products are as follows:

* They may block pores, causing irritation, or if applied to parietal surfaces,
granulomas, fibrosis or adhesions.
* There is a possibility of contamination: Starch, although an excellent dusting
powder, is organic and can support microbial growth. Talc, despite being an iCoating
mpound, can be contaminated with microorganisms and must therefore always be
sterilised prior to
incorporation into a dusting powder.
* Light fluffy powders may be inhaled by infants, causing breathing difficulties.
* They are not suitable for application to broken skin.

Some commonly used ingredients such as talc, kaolin and other natural mineral
substances are liable to be heavily contaminated with bacteria, including Clostridium
tetani, Clostridium welchii and Bacillus anthracis, which can cause tetanus and
gangrene. Therefore, such ingredients must have been sterilised before use. Dusting
powders are applied to the skin for a surface effect such as drying or lubrication.
Some dusting powders incorporate medicaments, giving them antibacterial or
antifungal action. Examples include:
* Talc Dusting Powder BP – Used as a lubricant to prevent chafing.
* Chlorhexidine Dusting Powder BP – Used for its antibacterial effect.
* Tinaderm Powder – A proprietary product used for the treatment of fungal infections
(e.g. Tinea infections such as athlete’s foot).

Common ingredients included in dusting powders and their

properties.

Absorbent
Bentonite BP
Kaolin BP
Starch BP
Talc BP

Dispersing and lubricating agents for ease of application

Starch BP
Talc BP

Adhesives that help the powder to stick to the skin

Aluminium Stearate BP
Magnesium Stearate BP
Zinc Stearate BP

Increase 'lightness and fluffiness'

Prepared Chalk BP
Zinc Stearate BP

White, with good covering properties

Talc BP
Zinc Oxide BP

Miscellaneous ingredients added to dusting powders:

Antibiotics
Boric Acid BP (not used in modern preparations)
Sulphur BP

Astringents
Aluminium Chloride BP
Tannic Acid BP

Cooling antipruritic ingredients

Camphor BP
Menthol BP
Thymol BP

Bulk oral powders

Bulk oral powders resemble dusting powders with the exception that they are intended
for oral administration. The dose to be taken is measured with a 5 mL spoon, stirred
into a quantity of water and then swallowed. Unfortunately, this method of
measurement creates considerable problems with regard to the expected standards of
precision of dosage. Preparations in this group are formulated on the basis of dose-
weights, whereas the dose is actually measured by volume. The measure of volume
used is a heaped 5 mL spoonful, which is considered to be the equivalent to 5 g of
powder. It is obvious that both the accuracy and precision of the dosage will be
significantly influenced by a large number of varying factors. These include the
density of the powders used, the interpretation of ‘heaped’ 5 mL spoon by the patient,
etc. Consequently, this formulation is restricted to use in preparations consisting of
relatively non-potent medicaments such as Kaolin BP and Magnesium Trisilicate BP,
where such products are intended for the symptomatic relief of minor ailments. Bulk
powders may be a single powder (e.g. Magnesium Trisilicate Powder BP) or a mix of
several powders (e.g. Calcium Carbonate Compound Powder BPC 1973). Common
proprietary products include Actonorm Powder, Andrews Salts, Bisodol Indigestion
Relief Powder and Eno Powder.

The advantages of bulk oral powders as pharmaceutical products are

that:
* dry powders may be more stable than their liquid equivalent
* large doses of bulky powders may be administered with relative ease (e.g.
indigestion powders)
* absorption from the gastrointestinal tract will be quicker than with capsules or
tablets.

The disadvantages of bulk oral powders as pharmaceutical products

are that:
* the accuracy of dosage is not guaranteed, therefore it is not a suitable dosage form
for potent medication
* the large size container means that they may be inconvenient to carry
* it is difficult to mask any unpleasant taste.

Individual unit dose powders

The sole difference between individual unit dose powders and bulk oral powders is
that the dosage problem is overcome by providing the patient with a set of separate
doses, each of which has been individually wrapped. Single-dose powders usually
consist of one or more powdered active medicaments, together with an inert diluent,
and wrapped as single doses in white demy paper, folded to a uniform shape and size.
The weight of each powder should be 200 mg, our recommended weight, for ease of
handling by the patient. This weight is chosen because:

* 200 mg can be weighed on a Class II balance (or electronic equivalent) (i.e. 200 mg
is greater than the minimum weighable quantity of the balance)

* 200 mg is an easy figure to use in pharmaceutical calculations (it is easy to

undertake calculations using multiples or divisions of 200)
* 200 mg is the amount of powder that will fit into a size 3 capsule and, for ease, it
would make sense to use the same calculations for both powders and capsules

The diluent used is normally Lactose BP as it is colourless, soluble and harmless and
therefore shows the ideal properties of an inert diluent. Starch BP is an alternative
diluent if the patient is lactose intolerant. Powders are useful for administration to
children who cannot swallow tablets. They may be taken by pouring onto the back of
the tongue and swallowing, or alternatively they may be added to a small amount of
water and swallowed. There are a number of proprietary brands of individual powders
of prescription-only medicines (POM) (e.g. Paramax Powders (paracetamol and
metoclopramide), Stemetil Powders (prochlorperazine)) and powders readily available
as over-the-counter (OTC) medicines include Beechams Powders, oral rehydration
sachets (Dioralyte), Fennings Children’s Cooling Powders and Resolve. Powders that
have been commercially manufactured are often packed in sealed sachets. This is
particularly true if they contain ingredients intended to produce effervescence, to
protect the contents from moisture.

The advantages of unit dose powders as pharmaceutical products are

as follows:
* They show greater stability than liquid dosage forms as the rate of reaction between
drugs in a dosage form in atmospheric conditions is slower than the rate of reaction in
a liquid medium.
* Accurate dosage is possible.
* They are easy to administer. Powders are relatively easy to swallow and may be
mixed with food or drink in order to assist administration.
* The small particle size leads to more rapid absorption from the gastrointestinal tract
compared with tablets. This in turn leads to reduced local irritation of the
gastrointestinal tract which may be caused by local concentration of a drug, as
encountered when taking an equivalent tablet.
* They are well accepted by patients, attractive to patients and convenient to carry.

The disadvantages of unit dose powders as pharmaceutical products

are as follows:
* They may be difficult to swallow.
* Unpleasant flavours, bitter or nauseous, are difficult to mask when in powder form.
Calculations for powders
There are two main calculations for powders, the choice being dependent on the
quantity of active ingredient to be incorporated into each powder and the total number
of unit doses (or excess) to be made. The two different calculations are termed single
dilution and double dilution (or serial dilution).

Single dilution
Write out the formula for one powder based on a final weighing of 200 mg. Then
write out the formula for the total number of powders. Remember to always make an
excess.
For example, if the prescription is for eight Furosemide 25 mg powders, including a
suitable excess, calculate for 10 powders:

For one powder for 10 powders

Furosemide BP 25 mg 250 mg
Lactose BP to 200 mg (i.e. 175 mg) to 2000 mg (i.e. 1750 mg)

So long as the final quantities to be weighed are above the minimum weighable
quantity of the balance single dilution can be used. In this case, 250 mg is the smallest
amount to be weighed. This is greater than the minimum weighable quantity of the
balance and so single dilution will be suitable. If, however, the amount of active
ingredient to be weighed is below the minimum weighable quantity of the balance,
double dilution must be used.

Double dilution (serial dilution)

When dosages of very potent drugs are required, the active ingredient will be present
in very low concentrations. By simply multiplying the quantities of the ingredients up
to weighable quantities, owing to the small amount of active ingredient that would be
present, it would be difficult to ensure that a uniform mix of active ingredient and
diluent would be obtained. This might result in ‘clumping’ of the active ingredient,
which could have potentially fatal consequences for the patient. The dosage at which
serial, rather than single, dilution would be required is to a certain extent arbitrary and
really a matter of professional judgement. Our suggested limit is that concentrations
of active ingredient below 15 mg require serial dilution. This limit is based on an
initial mix (including an excess) for 10 powders. If each powder contains 15 mg of
active ingredient, the total for 10 powders will be 150 mg of active ingredient (10 15
¼ 150). This (150 mg) is equal to the accepted usual minimum weighable quantity of
a Class II balance . Any smaller quantity would be less than the minimum weighable
quantity of the balance and therefore require double dilution. For example, if a
prescription is for five Bromocriptine powders 1 mg, a total for 10 powders should be
made:

For one powder. for10powders

Bromocriptine BP 1 mg. 10 mg

Lactose BP to 200 mg. to 2000 mg

However, the minimum recommended weight achievable on a Class II balance for

potent substances is 150 mg. This is 15 times more than the 10 mg required so single
dilution would not be suitable. Therefore, dilution with lactose is required, usually
based on multiples of 200 mg. Therefore if one part of bromocriptine = 200 mg then
200 mg is 19 times greater than the 10 mg required:
19 parts of lactose =19 200 mg =3800 mg

Let’s call this concentrate Mix X. Mix X is:

Bromocriptine BP 200 mg

Lactose BP 3800 mg

It is known that 200 mg of Mix X will contain the 10 mg of Bromocriptine BP

required for the master formula. Master formula for 10 powders:

Bromocriptine BP 10 mg. =Mix X 200 mg

Lactose BP. =to 2000 mg
(i.e. 1990 mg) (i.e. 1800 mg)

This will provide 10 powders each containing 10 mg of Bromocriptine BP.

Unit dose capsules

Capsules are a further development from unit dose powders in that each dose of
powder is enclosed in an edible container, which is swallowed whole with a
draught of water (about 30–60 mL). The powder is not released from its container
until it is in the stomach. This type of presentation is more convenient for the patient,
and is particularly useful for medicaments which have an unpleasant taste. The
advantages and disadvantages of unit dose capsules are similar to those of unit dose
powders.

The advantages of unit dose capsules as pharmaceutical products are

as follows:
* They are stable. Powders show greater stability than liquid dosage forms as the rate
of reaction between drugs in a dosage form in atmospheric conditions is slower than
the rate of reaction in a liquid medium.
* Accurate dosage is possible.
* They are easy to administer – capsules are relatively easy to swallow (suitable shape
and slippery when moistened).
* Unpleasant tastes can be easily masked.
* The release characteristics of the drugs can be controlled.
* They can be made light resistant using opaque capsules.
* The smaller particle size of powdered drugs leads to more rapid absorption from the
gastrointestinal tract compared to tablets. This in turn leads to reduced local irritation
of the gastrointestinal tract which may be caused by local concentration of a drug as
encountered when taking an equivalent tablet. They are well accepted by patients,
attractive to patients and convenient to carry.

The disadvantages of unit dose capsules as pharmaceutical products

are as follows:
* They may be difficult to swallow.
* Capsules are unsuitable for very small children.
* Patients with strict religious beliefs and vegetarians may object to the use of animal
gelatin (although non-animal gelatin capsules may be available)

There are two main basic types of capsule:

Soft gelatin capsules – These are flexible capsules and may be spherical, ovoid or
cylindrical in shape. They are usually used in manufacturing when they are formed,
filled and sealed in one operation. Examples of this type of capsule include Atromid
S, Efamast, Epogam and nifedipine capsules (they tend to be used mainlyfor oils,
gels, etc.).

Hard capsules – These are made of hard gelatin and formed in two halves. The
medicament is inserted into the longer portion and the second half fitted. Patients
should be instructed to swallow the capsules whole and NOT to open them. Hard
gelatin capsules are available in a variety of different sizes.

Approximate capacities of capsules

Size of capsule Contents (mg)
000 950
00 650
0 450
1 300
2 250
3 200
4 150
5 100

TABLET DOSAGE FORM

Introduction-
• According to USP, Tablet is defined as a compressed solid dosage form containing
medicaments with or without Excipients.
• According to the Indian Pharmacopoeia, Pharmaceutical tablets are solid, flat or
biconvex dishes, unit dosage form, prepared by compressing a drug or a mixture of
drugs, with or without diluents

Advantages of tablet dosage form over other oral drug delivery systems

From patients stand point:

• They are easy to carry, easy to swallow and they are attractive in appearance.
• Unpleasant taste can be masked by sugar coating and they do not require any
measurement of dose.
• Some of the tablets are divided into halves and quarters by drawing lines during
manufacturing to facilitate breakage whenever a fractional dose is required.

From the standpoint of manufacturer:

• An accurate amount of medicament, even if very small, can be incorporated.
• Tablets provide best combined properties of chemical, mechanical and
microbiological stability of all the oral dosage forms.
• Since they are generally produced on a large scale, therefore, their cost of production
is relatively low, hence economical.
• They are in general the easiest and cheapest to package and ship among all oral
dosage forms.
• Some specialized tablets may be prepared for modified release profile of the drug.
• Product identification is potentially the simplest and cheapest requiring no additional

processing steps when employing an embossed or monogrammed punch face.

Disadvantages of tablet dosage form

1. Difficult to swallow in case of children and unconscious patients.
2. Drugs with poor wetting, slow dissolution properties, optimum absorption high in
GIT
may be difficult to formulate or manufacture as a tablet that will still provide adequate

or full drug bioavailability.

3. Bitter testing drugs, drugs with an objectionable odor or drugs that are sensitive to
4. oxygen may require encapsulation or coating. In such cases, capsule may offer the
best and lowest cost.
5.Some drugs resist compression into dense compacts, owing to amorphous nature,
low
density character.

Types of tablets-
(a) Tablets ingested orally:
• Compressed tablets
• Multiple compressed tablets
• Enteric coated tablets
• Sugar coated tablets
• Film coated tablets
• Chewable tablets

(b) Tablets used in the oral cavities:

• Buccal Tablets
• Sublingual tablets
• Lozenges
• Dental cones

(c) Tablets administered by other routes:

• Implantation tablets
• Vaginal tablets

(d) Tablets used to prepare solutions:

• Effervescent tablets
• Dispensing tablets
• Hypodermic tablets
• Tablet triturates

(a) Tablets ingested orally-

(1) Compressed tablets:-
• These tablets are formed by compression and contain no special coating. They are
made from powdered, crystalline or granular materials, alone or in combination with
suitable excipients. These tablets contain water soluble drugs which after swallowing
get disintegrated in the stomach and its drug contents are absorbed in the
gastrointestinal tract and distributed in the whole body. e.g. Aspirin (Dispirin)
paracetamol tablets (Crocin).

(2) Multiple compressed tablets / Layered tablets-

These are compressed tablets made by more than one compression cycle. Such tablets

are prepared by compressing additional tablet granulation on a previously compressed

granulation. The operation may be repeated to produce multilayered tablets of two or
three layers. To avoid incompatibility, the ingredients of the formulation except the
incompatible material are compressed into a tablet and then incompatible substance
along with necessary excipients are compressed over the previously compressed
tablet.

(3) Sustained action tablets:

These are the tablets which after oral administration release the drug at a desired time
and prolong the effect of the medicament. These tablets when taken orally release the
medicament in a sufficient quantity as and when required to maintain the maximum
effective concentration of the drug in the blood throughout the period of treatment.
e.g. Diclofenac SR tablets.

(4) Enteric coated tablets:

These are compressed tablet meant for administration by swallowing and are
designed
to by-pass the stomach and get disintegrated in the intestine only. These tablets are
coated with materials resistant to acidic pH (like cellulose acetate phthalate, CAP) of
the gastric fluid but get disintegrated in the alkaline pH of the intestine.

(5) Sugar coated tablets:

These are compressed tablets containing a sugar coating. Such coatings are done to
mask the bitter and unpleasant odour and the taste of the medicament. The sugar
coating makes the tablet elegant and it also safeguard the drug from atmospheric
effects.

(6) Film coated tablets:

The compressed tablets having a film coating of some polymer substance, such as
hydroxy propyl cellulose, hydroxy propyl methyl cellulose and ethyl cellulose. The
film coating protects the medicament from atmospheric effects. Film coated tablets
are
generally tasteless, having little increase in the tablet weight and have less elegance
than that of sugar coated tablets.

(7) Chewable tablets:

These are the tablets which are required to be broken and chewed in between the teeth

before ingestion. These tablets are given to the children who have difficulty in
swallowing and to the adults who dislike swallowing. These tablets should have very
acceptable taste and flavour. Ex- Antacid tablets (Digiene).

(b) Tablets used in oral cavity

(1) Buccal tablets:
These tablets are to be placed in the side of the cheek (buccal pouch) where they
dissolve or erode slowly and are absorbed directly in the buccal cavity without
passing
into the alimentary canal. Therefore, they are formulated and compressed with
sufficient pressure to give a hard tablets. e.g. Progesterone tablets.

(2) Sublingual tablets:

These tablets are to be placed under the tongue where they dissolve or disintegrate
quickly and are absorbed directly without passing into GIT. e.g. tablets of
nitroglycerin,
isoproterenol hydrochloride or erythrityl tetranitrate.

(3) Lozenges tablets:

These tablets are designed to exert a local effect in the mouth or throat. These tablets
are commonly used to treat sore throat to control coughing in common cold. They
may
contain local anaesthetics, antiseptics, antibacterial agents and astringents. These are
prepared by compression at a high pressure by the moulding process and generally
contain a sweetening agent, flavouring agent and a substance which roduces a cooling
effect. e.g. Vicks lozenges, Strepsils.

(4) Dental cones:

These are compressed tablets meant for placement in the empty sockets after tooth
extraction. They prevent the multiplication of bacteria in the socket following such
extraction by using slow-releasing antibacterial compounds or to reduce bleeding by
containing the astringent.These tablets contain an excipient like lactose, sodium
bicarbonate and sodium chloride. These cones generally get dissolved in 20 to 40
minutes time.

(c) Tablets administered by other routes

(1) Implantation Tablets:
These tablets are placed under the skin or inserted subcutaneously by means of minor
surgical operation and are slowly absorbed. These may be made by heavy
compression
but are normally made by fusion. The implants must be sterile and should be packed
individually in sterile condition. Implants are mainly used for the administration of
hormones such as testosterone steroids for contraception. These tablets are very
usefully exploited for birth control purpose in human beings. The disadvantages of
implant tablets are their administration, changing rate of release with change of
surface area and possibility of tissue reactions.

(2) Vaginal tablets:

These tablets are meant to dissolve slowly in the vaginal cavity. The tablets are
typically
ovoid or pear shaped for the ease of insertion. these tablets are used to release steroids

or antimicrobial agents. the tablets are often buffered to promote a pH favorable to the

action of a specified antimicrobial agent. The contains easily soluble components like
lactose or sodium bicarbonate.

Tablets used to prepare solutions

(1) Effervescent tablets:
These tablets along with the active medicament contain ingredients like sodium
bicarbonate, citric acid and tartaric acid which react in the presence of water liberating
carbon dioxide and producing effervescence leading to disintegration of the tablet,
thus
fastens solution formation and increase the palatability. Eg. Histac (Ranitidine)

(2) Dispensing tablets:

These tablets provide a convenient quantity of potent drug that can be readily convert
into powders and incorporate into liquids, thus circumventing the necessity to weigh
small quantities. these tablets are supplied primarily as a convenience for
extemporaneous compounding and should never be dispensed as dosage form. e.g.
The drugs commonly incorporated are mild silver potentiate, bichloride of mercury
merbromin an quarternary ammonium compounds.

(3) Hypodermic tablets:

Hypodermic tablets are soft, readily soluble tablets and originally were used for the
preparation of solutions to be injected. These tablets are dissolved in sterile water or
water for injection and administered by parenteral route. these tablets are not
preferred
now-a-days because the resulting solution is not always sterile.

(4) Tablet triturates (Moulded tablets):

These are powders moulded into tablets. They are flat, circular discs, usually
containing
a potent substance mixed with lactose, lactose and sucrose, dextrose, or other suitable
diluent. Since they are intended to disintegrate very quickly in contact with moisture,
water insoluble adjuncts are avoided. The name ‘tablet triturate’ is appropriate
because they usually contain triturations (trituration = dilution with an inert
substance).

Tablet Ingredients/ Excipients-

In addition to active ingredients, tablet contains a number of inert materials known as
additives or excipients. Different excipients are:
1. Diluent / Filler
2. Binder and adhesive
3. Disintegrants
4. Lubricants and glidants
5. Colouring agents
6. Flavoring agents
7. Sweetening agents

Function of excipients-
1. Impart weight, accuracy, & volume.
2. Improve solubility
3. Increase stability
4. Enhance bioavailability
5. Modifying drug release
6. Assist product identification
7. Increase patient acceptability
8. Facilitate dosage form design

1. Diluents
Definition- Diluents are fillers used to make required bulk of the tablet when the drug
dosage itself is inadequate to produce the bulk. Secondary reason is to provide better
tablet properties such as improve cohesion, to permit use of direct compression
manufacturing or to promote flow.

A diluent should have following properties:

1. They must be non-toxic and low cost.
2. They must be commercially available in acceptable grade
3. They must be physiologically inert, physically & chemically stable by themselves
& in combination with the drugs.
4. They must be free from all microbial contamination.
5. They do not alter the bioavailability of drug.
6. They must be color compatible.

Characteristics of an ideal diluents

• They must be nontoxic and acceptable to the regulatory agencies in all countries
where the product is to be marketed.
• They must be commercially available in an acceptable grade in all countries where
the
product is to be manufactured.
• They must be cheap compared to the active ingredients and must be physiologically
inert.
• They must be chemically stable alone and/or in combination with the drug(s) and/or
other tablet components.
• They must be color-compatible (should not produce any off-color appearance).
• They must have no negative effects on the bioavailability of the drug(s) in the
product
Commonly used tablet diluents-

1- Lactose-anhydrous and spray dried lactose

2. Directly compressed starch-Sta Rx 1500
3. Hydrolyzed starch-Emdex and Celutab
4. Microcrystalline cellulose-Avicel (PH 101and PH 102)
5. Dibasic calcium phosphate dehydrate
6. Calcium sulphate dihydrate
7. Mannitol and Sorbitol
8. Sucrose- Sugartab, DiPac, Nutab
9. Dextrose

2. Binders and Adhesive

Definition- Agents used to impart cohesive qualities to the powdered material are
referred to as binders or granulators.Objective of incorporating binders
• They impart a cohesiveness to the tablet formulation (both direct compression and
wet–granulation method) which insures the tablet remaining intact after compression.
• They improves the free-flowing qualities by the formation of granules of desired
size
and hardness.
Examples of binders
1. Starch paste
2. Corn starch is often used in the concentration of 10–20%.
3. Liquid glucose:- 50% solution in water is fairly common binding agent.
4.Sucrose solution:- 50% to 74% sugar solution is used as binder. They produce hard
but brittlegranules. Their cost is low.
5. Gelatin solution
• Concentration 10–20% aqueous solution

3. Disintegrants
Definition:- A disintegrant is a substance to a mixture of substances, added to tablet to
facilitateits breakup or disintegration after administration in the GIT. The active
ingredients must be released from the tablet matrix as efficiently as possible to allow
for its rapid dissolution. Disintegrants can be classified chemically as: Starches, clays,
celluloses, alginates, gums and cross-linked polymers.

Starch

• Corn starch, potato starch.

• For their disintegrating effect starches are added to the powder blends in dry state.
Mode of action:

• Starch has a great affinity for water and swells when moistened, thus facilitating the
rupture of the tablet matrix.
• Others have suggested that the spherical shape of the starch grains increases the
porosity of the tablet, thus promoting capillary action.
• Normally 5% w/w is suggested and for rapid disintegration 10 – 15% w/w may be
taken. Superdisintegrants Super disintegrants like Croscarmelose - cross linked
cellulose, Crospovidone - cross linked polyvinyl pyrrolidone and Sodium starch
glycolate- cross linked starch

Mode of action
• Croscarmelose swells 4 to 8 fold in less than 10 seconds

4. Lubricant and Glidants

Objectives:
• Prevents adhesion of the tablet material to the surface of dies and punches.
• Reduce inter-particular friction, improve the rate of flow of tablet granulation.
• Facilitate ejection of the tablets from the die cavity.
Lubricants are intended to prevent adhesion of the tablet materials to the surface of
dies and punches, reduce inter particle friction and may improve the rate of flow of
the tablet
granulation.
Example: Stearic acid, Stearic acid salt - Stearic acid, Magnesium stearate, Talc, PEG
(Polyethylene glycols), Surfactants.
Glidants are intended to promote flow of granules or powder material by reducing the
friction
between the particles.
Example: Corn Starch – 5-10% conc., Talc-5% conc., Silica derivative - Colloidal
silicas such as Cab-O- Sil, Syloid, Aerosil in 0.25-3% conc.

Antiadherents are used for the purpose of reducing the sticking or adhesion of any of
the tablet ingredients or powder to the faces of the punches or to the die wall.

5. Coloring agent

Objectives of using colors that (i) It makes the tablet more esthetic in appearance and
(ii) Colour helps the manufacturer to identify the product during its preparation.
Colorants are obtained in two forms dyes and lakes. Dyes are dissolved in the binding
solution prior to the granulating process. However, duringdrying their color may
migrate to the surface and may produce mottling of the tablet. So another approach is
to adsorb the dye on starch or calcium sulfate from its aqueous solution; the resultant
powder is dried and blended with other ingredients. Color lakes are dyes which are
adsorbed onto a hydrous oxide of a heavy metal (likealuminium) resulting in an
insoluble form of the dye.

6. Flavours and Sweeteners

Flavours are usually limited to chewable tablets or other tablets intended to dissolve
in the mouth. Flavor oils are added to tablet granulations in solvents, are dispersed on
clays and other adsorbents or are emulsified in aqueous granulating agents (i.e.
binder).
The use of sweeteners is primarily limited to chewable tablets. E.g. Sugar
• Mannitol– 72% as sweet as sugar, cooling & mouth filling effect
• Saccharin– Artificial sweetener, 500 times sweeter than sucrose

Disadvantages (i) it has a bitter after taste and (ii) carcinogenic

• Cyclamate– either alone or with saccharin– it is banned
• Aspartame (Searle) – widely replacing saccharin
Disadvantage – lack of stability in presence of moisture

Manufacturing of Tablets
Manufacture of tablets involves certain well defined steps: namely:-
1.Pulverization and mixing.
2.Granulation.
3.Compression.
4.Coating (if required)

1. Pulverization and mixing-

• In this step the different solid / powder ingredients are reduced to the same particle
size since particles of different sizes will segregate while mixing.
• Various equipments like Cutter mill, Hammer mill, Roller mill and Fluid energy mill
is required to reduce the large lumps.

2.Granulation. It is the process in which primary powder particles are made to

adhere to form large multi-particle entities. Range of size: 0.2 mm to 4 mm. (0.2 mm
to 0.5 mm)

Objectives:-
1.To enhance the flow of powder.
2.To produce dust free formulations and produce uniform mixtures.
3.To improve compaction characteristics.
4.To eliminate poor content uniformity of mix.
5.To avoid powder segregation. As Segregation may result in weight variation.

Types of Granulation.
(a) Wet Granulation
This type requires addition of liquid binder before the granules are produce as such
the granules produced must be dried.
(b) Dry Granulation
Dry granulation is followed in situations where (i) the effective dose of a drug is too
high
for direct compaction and (ii) if the drug is sensitive to heat, moisture or both, which
precludes wet granulation. e.g. many aspirin and vitamin formulations are prepared
for
tableting by compression granulation.

3. Tablet Compression
It can reduce the volume by apply pressure, particle in die are re-arrange, resulting a
closer packing structure and reduce space and at certain lode reduced space and
increase interparticulate friction will prevent farther interparticulate friction.

Basic Component of Compression Machine

Head- Contain upper punchs, dies, lower punchs.
Body- Contain operating machinaries.
Hopper- Holding feeding granules.
Dies- Define size, shape of tablet.
Punches – For compression with in dies.
Cam tracks – Guiding the movement of punches.
Feed frame- Guiding the granules from hopper to dies.
Upper turret- Holds the upper punchs.
Lower turret- Hold the lower punchs.
Die table- Contain the dies.

Types o tabletting machine

1. Single station – stamping press
2. Multi- station- Rotary press

4. Tablets Coating
Reasons Behind Coating of Tablets:
To mask the taste, odour or colour of the drug. Improving the product appearance,
particularly where there are visible differences in tablet core ingredients from batch to

batch.
1. To Provide physical protection, facilitates handling, particularly in high speed
packaging / filling lines.
2. To provide chemical protection from its surrounding environment (particularly
air,
moisture and light).
3. To control the release of drug from the tablet e.g. sustained release tablets, repeat
action tablets.
4.To protect the drug from the gastric environment of the stomach with an acid
resistant enteric coating.

Components Considered in Tablet Coating

Tablet Properties: - Shape, Tolerance, Surface area.
1.Tablet to be coated must possess the proper physical characteristics like spherical
shape and uniform surface.
2.To tolerate attrition of tablets during coating process they must be resistant to
abrasion and chipping.
3.As the tablet surfaces that are brittle and soften in presence of heat or effected by
coating composition and tend to become rough in the early stages of coating process
are unacceptable for film coating.

Types of Coating-
(A) Sugar Coating.
(B) Film Coating
(C) Enteric Coating